Synthesis and antiproliferative activity in vitro of diacetylenic thioquinolines.

A series of new acetylenic thioquinolines containing propargyl, 2-butynyl, or 4-bromo-2-butynyl groups has been prepared and tested for antiproliferative activity in vitro against the cells of human [SW707 (colon cancer), CCRF/CEM (leukemia)] and murine [P388 (leukemia), B16 (melanoma)] cancer lines. All the compounds obtained exhibited antiproliferative activity. The most active compounds 4h and 41-m have ID 50 values ranging from 0.2 to 3.6 μg/ml, comparable to that of the reference compound cisplatin.